| Vacquinol-1MAPK kinase 4 (MKK4) activator |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
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| Cas No. | 5428-80-8（free base） | SDF | Download SDF |
| Chemical Name | (2-(4-chlorophenyl)quinolin-4-yl)(piperidin-2-yl)methanol | ||
| Canonical SMILES | OC(C1=CC(C2=CC=C(Cl)C=C2)=NC3=CC=CC=C13)C4NCCCC4 | ||
| Formula | C21H23Cl3N2O | M.Wt | 425.78 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: 3.14 μM for glioma cells
Vacquinol-1 is a MAPK kinase 4 (MKK4) activator.
Mitogen-activated protein kinase (MAPK) is a type of protein kinase that is specific to the amino acids serine, threonine, and tyrosine. MAPKs regulate cell functions such asgene expression, mitosis, proliferation, differentiation, cell survival, as well as apoptosis.
In vitro: Previous study showed that vacquinol-1 displayed high cytotoxicity against glioma cells, resulting in a complete loss of viability as measured by ATP depletion. Vacquinol-1 could selectively target GCs in mixed cocultures with human fibroblasts. Moreover, vacquinol-1 had no effect on caspase activity at any concentration or time point, which was unlike that of staurosporin. In addition, the fluorescence staining and western blot analyses of GCs for activating MKK4 phosphorylation revealed a rapid and pronounced activation by vacquinol-1 at 7.5 μM [1].
In vivo: The ability of vacquinol-1 to attenuate tumor progression was previously tested in a mouse model for human GBM. Vacquinol-1 or vehicle (DMSO) were intracranially administered into the site of original cell deposit 6 weeks after engraftment. Results showed that tumors were invariantly smaller, and the area of necrosis and hGFAP and hNestin immunoreactivity was significantly reduced. Moreove, only tumor cells in vacquinol-1-treated mice showed a massive LAMP1 staining [1].
Clinical trial: Up to now, vacquinol-1 is still in the preclinical development stage.
Reference:[1] Kitambi SS et al. Vulnerability of glioblastoma cells to catastrophic vacuolization and death induced by a small molecule. Cell. 2014 Apr 10;157(2):313-28.
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组织处理主要有批评教育、通报批评、调离、降职、责令辞职、免职等形式。
这样子好吗？我个人认为理论上问题不大，不知道是不是
我现在做药物动力学中的组织分布部分试验，现在遇到了难题，就是肝脏组织太脏，不知道该如何处理才能上样呢？谢谢！！
还有就是想请教各位老师，小鼠尾静脉注射有什么技巧呢？我有时候能打进去，有时候打到组织中啦，谢谢各位大师指点迷津。
